Source:http://linkedlifedata.com/resource/pubmed/id/19850473
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
23
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pubmed:dateCreated |
2009-11-5
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pubmed:abstractText |
Cannabinoid CB-1 receptors have been the focus of extensive studies since the first clinical results of rimonabant (SR141716) for the treatment of obesity and obesity-related metabolic disorders were reported in 2001. To further evaluate the properties of CB receptors, we have designed and efficiently prepared a series of pentacycle derivatives. Five of the new compounds which displayed high in vitro rCB1 binding affinities were assayed for binding to hCB2 receptor. Noticeably, 2-(5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-(5-methyl-1,3,4-thiadiazol-2-yl)-1H-pyrazol-3-yl)-5-(1-(trifluoromethyl)cyclopropyl)-1,3,4-oxadiazole (16l) demonstrated good binding affinity and decent selectivity for rCB1 receptor (IC(50)=1.72 nM, hCB2/rCB1=142).
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6632-6
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pubmed:meshHeading |
pubmed-meshheading:19850473-Animals,
pubmed-meshheading:19850473-Drug Design,
pubmed-meshheading:19850473-Humans,
pubmed-meshheading:19850473-Ligands,
pubmed-meshheading:19850473-Molecular Structure,
pubmed-meshheading:19850473-Pyrazoles,
pubmed-meshheading:19850473-Rats,
pubmed-meshheading:19850473-Receptor, Cannabinoid, CB1,
pubmed-meshheading:19850473-Stereoisomerism,
pubmed-meshheading:19850473-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
Pentacycle derivatives as cannabinoid CB1 receptor ligands.
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pubmed:affiliation |
Central Research Laboratories, Green Cross Corporation, Yongin, Gyeonggi-Do 446-770, Republic of Korea.
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pubmed:publicationType |
Journal Article
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